Many natural products or bio-molecules contain α-amino acid or α-amino alcohol units in their structures. While these units may be obtained from naturally occurring α-amino acids, general methods to obtain other non-natural α-amino acids are highly sought-after. Direct synthesis of α-amino acids from air by means of biomimetic methods has been regarded as one of the most challenging tasks. The biological method involving copper enzymatic activation of dioxygen has attracted considerable attention, owing to the existence of important copper mono-oxygenases. Mimicking this system to study copper-dioxygen interactions and further applications of dioxygen-copper systems in organic synthesis, especially in the developments of aliphatic C—H bond oxidation or C—H bond amination chemistry, has attracted tremendous interest. For C—H bond activation, dioxygen-copper systems provide an alternative to the commonly employed methods which use expensive metal catalysts and stoichiometric metal oxidants.